养殖与饲料2024年第5期酮康唑⁃甲基⁃β⁃环糊精包合物的表征及抑菌活性研究徐淑凤，张志远，马艳芝，聂结华，廖洁丹*佛山科学技术学院生命科学与工程学院，广东佛山528225摘要［目的］为了提高低水溶性抗真菌药物酮康唑（ketoconazole，KCZ）的水溶性及抑菌活性，减少临床应用限制。［方法］采用饱和溶液法制备酮康唑-甲基-β-环糊精包合物，高效液相色谱法（HPLC）检测其溶解度，通过傅里叶变换红外光谱（IR）法对其结构进行表征，用纸片扩散法（K-B法）和最小抑菌浓度(MIC)方法对比检验酮康唑原药与酮康唑-甲基-β-环糊精包合物对白色假丝酵母菌的体外抗菌活性。［结果］通过甲基-β-环糊精包合，酮康唑在包合物中的水溶性比单一酮康唑增加了约2941倍，通过傅里叶变换红外光谱（IR）法证实了有新物相形成。酮康唑原药的抑菌圈为（22.00±1.63）mm，酮康唑-甲基-β-环糊精包合物的抑菌圈则提升至（28.00±1.63）mm。最低抑菌浓度结果显示，酮康唑原药的最低抑菌浓度为（0.125±0.029）μg/mL，酮康唑-甲基-β-环糊精包合物的最低抑菌浓度为（0.0625±0.0150）μg/mL。［结论］酮康唑-甲基-β-环糊精包合物不仅没有破坏酮康唑原药对白色假丝酵母菌原有的抑菌能力，还提高了其抑菌效果。关键词酮康唑；包合物；傅里叶变换红外光谱；药敏试验；最小抑菌浓度Characterizingtheinclusioncomplexofketoconazole-methyl-Characterizingtheinclusioncomplexofketoconazole-methyl-β-cy-cy‐clodextrinanditsantibacterialactivityclodextrinanditsantibacterialactivityXUShufeng,ZHANGZhiyuan,MAYanzhi,NIEJiehua,LIAOJiedan*CollegeofLifeScienceandEngineering,FoshanUniversity,Foshan528225,ChinaAbstractAbstract[Objectives]Inordertoimprovethewatersolubilityandantibacterialactivityofthelowwater-solubleantifungaldrugketoconazole(KCZ)andreducethelimitsofclinicalapplication.[Methods]Theinclusioncomplexofketoconazole-methyl-β-cyclodextrinwaspreparedwiththesatu‐ratedsolutionmethod.Thewatersolubilityoftheinclusioncomplexwasmeasuredwithhigh-performanceliquidchromatography(HPLC).Fouriertransforminfraredspectroscopy(IR)wasusedtocharacterizethestructureoftheinclusioncomplex.Theinvitroantibacterialactivityofthesingleketo‐conazoleandtheinclusioncomplexofketoconazole-methyl-β-cyclodextrinagainstCandi...
